JP2019518779A5 - - Google Patents
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- Publication number
- JP2019518779A5 JP2019518779A5 JP2018567299A JP2018567299A JP2019518779A5 JP 2019518779 A5 JP2019518779 A5 JP 2019518779A5 JP 2018567299 A JP2018567299 A JP 2018567299A JP 2018567299 A JP2018567299 A JP 2018567299A JP 2019518779 A5 JP2019518779 A5 JP 2019518779A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- compound
- pharmaceutically acceptable
- alkyl
- halogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims description 87
- 239000001257 hydrogen Substances 0.000 claims description 87
- 150000001875 compounds Chemical class 0.000 claims description 70
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 51
- 229910052736 halogen Inorganic materials 0.000 claims description 38
- 150000002367 halogens Chemical class 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 37
- 150000002431 hydrogen Chemical class 0.000 claims description 36
- 239000012453 solvate Substances 0.000 claims description 34
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 29
- 125000001188 haloalkyl group Chemical group 0.000 claims description 29
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- 208000035475 disorder Diseases 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 9
- 125000002252 acyl group Chemical group 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 9
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 9
- 125000004995 haloalkylthio group Chemical group 0.000 claims description 9
- 239000003937 drug carrier Substances 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims description 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 3
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 3
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 3
- 208000032781 Diabetic cardiomyopathy Diseases 0.000 claims description 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 3
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 3
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims description 3
- 102000016912 Aldehyde Reductase Human genes 0.000 claims description 2
- 108010053754 Aldehyde reductase Proteins 0.000 claims description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 2
- 239000011575 calcium Substances 0.000 claims description 2
- 229910052791 calcium Inorganic materials 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000007166 healthy aging Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 229910052744 lithium Inorganic materials 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- 239000011591 potassium Substances 0.000 claims description 2
- 229910052700 potassium Inorganic materials 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- 230000001737 promoting effect Effects 0.000 claims description 2
- 208000017520 skin disease Diseases 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- -1 tetrafluoroborate Chemical compound 0.000 claims description 2
- 230000000451 tissue damage Effects 0.000 claims description 2
- 231100000827 tissue damage Toxicity 0.000 claims description 2
- 239000011701 zinc Substances 0.000 claims description 2
- 229910052725 zinc Inorganic materials 0.000 claims description 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 0 *c1c(*)c(*)c(C=*)c(*C=*)c1* Chemical compound *c1c(*)c(*)c(C=*)c(*C=*)c1* 0.000 description 5
- 239000000758 substrate Substances 0.000 description 2
- DSDSUBSQMWKTBH-GSLILNRNSA-N CC(CO)[C@H]([C@@H]([C@H](CN(C)C)O)O)O Chemical compound CC(CO)[C@H]([C@@H]([C@H](CN(C)C)O)O)O DSDSUBSQMWKTBH-GSLILNRNSA-N 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-O NC(CCCNC(N)=[NH2+])C(O)=O Chemical compound NC(CCCNC(N)=[NH2+])C(O)=O ODKSFYDXXFIFQN-UHFFFAOYSA-O 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021094883A JP7368419B2 (ja) | 2016-06-21 | 2021-06-07 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2023176883A JP7688681B2 (ja) | 2016-06-21 | 2023-10-12 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2025086125A JP2025124733A (ja) | 2016-06-21 | 2025-05-23 | アルドース還元酵素阻害剤およびその使用方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662352784P | 2016-06-21 | 2016-06-21 | |
| US62/352,784 | 2016-06-21 | ||
| PCT/US2017/038505 WO2017223179A1 (en) | 2016-06-21 | 2017-06-21 | Aldose reductase inhibitors and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021094883A Division JP7368419B2 (ja) | 2016-06-21 | 2021-06-07 | アルドース還元酵素阻害剤およびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019518779A JP2019518779A (ja) | 2019-07-04 |
| JP2019518779A5 true JP2019518779A5 (enExample) | 2020-07-27 |
| JP6895464B2 JP6895464B2 (ja) | 2021-06-30 |
Family
ID=60783884
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018567299A Active JP6895464B2 (ja) | 2016-06-21 | 2017-06-21 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2021094883A Active JP7368419B2 (ja) | 2016-06-21 | 2021-06-07 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2023176883A Active JP7688681B2 (ja) | 2016-06-21 | 2023-10-12 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2025086125A Pending JP2025124733A (ja) | 2016-06-21 | 2025-05-23 | アルドース還元酵素阻害剤およびその使用方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021094883A Active JP7368419B2 (ja) | 2016-06-21 | 2021-06-07 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2023176883A Active JP7688681B2 (ja) | 2016-06-21 | 2023-10-12 | アルドース還元酵素阻害剤およびその使用方法 |
| JP2025086125A Pending JP2025124733A (ja) | 2016-06-21 | 2025-05-23 | アルドース還元酵素阻害剤およびその使用方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (6) | US10150779B2 (enExample) |
| EP (3) | EP4316603A3 (enExample) |
| JP (4) | JP6895464B2 (enExample) |
| CN (2) | CN109310674B (enExample) |
| AU (4) | AU2017281082B2 (enExample) |
| CA (1) | CA3025081A1 (enExample) |
| DK (2) | DK3757107T3 (enExample) |
| ES (2) | ES2966094T3 (enExample) |
| FI (1) | FI3757107T3 (enExample) |
| HR (2) | HRP20231563T1 (enExample) |
| HU (2) | HUE064911T2 (enExample) |
| IL (3) | IL283809B2 (enExample) |
| LT (2) | LT3757107T (enExample) |
| MX (2) | MX391561B (enExample) |
| PL (1) | PL3757107T3 (enExample) |
| PT (2) | PT3757107T (enExample) |
| RS (1) | RS61239B1 (enExample) |
| SG (2) | SG11201810642XA (enExample) |
| SI (2) | SI3352754T1 (enExample) |
| WO (1) | WO2017223179A1 (enExample) |
| ZA (1) | ZA201808506B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8916563B2 (en) | 2010-07-16 | 2014-12-23 | The Trustees Of Columbia University In The City Of New York | Aldose reductase inhibitors and uses thereof |
| IL283809B2 (en) * | 2016-06-21 | 2024-01-01 | Univ Columbia | Compounds for use in a method of treating neuropathy, retinopathy, nephropathy, or cardiomyopathy |
| IL272246B2 (en) * | 2017-07-28 | 2026-01-01 | Applied Therapeutics Inc | History of 2-(4-oxo/thioketone/azo-3-((substituted)benzo[d]thiazol-2-yl)methyl)- 3,4-dihydrothieno[3,4-d]pyridazin-1-yl)acetic acid for use as an aldose reductase inhibitor for the treatment of galactosemia or prevention of galactosemia-related complications |
| WO2020167937A1 (en) * | 2019-02-12 | 2020-08-20 | Applied Therapeutics, Inc. | Methods for treating cutaneous aging |
| AU2020254610A1 (en) * | 2019-04-01 | 2021-11-18 | Applied Therapeutics Inc. | Inhibitors of aldose reductase |
| CN113966396A (zh) | 2019-05-07 | 2022-01-21 | 迈阿密大学 | 遗传性神经病和相关障碍的治疗和检测 |
| IL291946A (en) * | 2019-10-08 | 2022-06-01 | Applied Therapeutics Inc | Aldose reductase inhibitors for the treatment of phosphomannomutase 2 deficiency |
| EP4125909A1 (en) | 2020-03-31 | 2023-02-08 | Applied Therapeutics Inc. | Aldose reductase inhibitors for the treatment of acute respiratory distress syndrome, acute lung inflammation/injury, cardiac injury and anti-viral therapy |
| CN115996725A (zh) * | 2020-05-01 | 2023-04-21 | 应用治疗公司 | 用于治疗山梨糖醇脱氢酶缺乏症的醛糖还原酶抑制剂 |
| WO2022197487A1 (en) * | 2021-03-18 | 2022-09-22 | Banavara MYLARI | Combination of aldose reductase inhibitors and probenecid for the treatment of diabetic complications |
| WO2025219948A1 (en) | 2024-04-17 | 2025-10-23 | Assia Chemical Industries Ltd. | Crystalline forms of govorestat |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0189272A3 (en) * | 1985-01-17 | 1987-08-19 | Fujisawa Pharmaceutical Co., Ltd. | New furanone derivatives, processes for preparation thereof and use thereof |
| CA1299178C (en) | 1985-11-07 | 1992-04-21 | Banavara Lakshmana Mylari | Heterocyclic oxophtalazinyl acetic acids |
| US4939140A (en) | 1985-11-07 | 1990-07-03 | Pfizer Inc. | Heterocyclic oxophthalazinyl acetic acids |
| ES2032749T3 (es) | 1985-11-07 | 1993-03-01 | Pfizer Inc. | Acidos oxoftalazinil-aceticos heterociclicos. |
| US4868301A (en) * | 1987-06-09 | 1989-09-19 | Pfizer Inc. | Processes and intermediates for the preparation of oxophthalazinyl acetic acids having benzothiazole or other heterocyclic side chains |
| WO1989006651A1 (en) | 1988-01-19 | 1989-07-27 | Pfizer Inc. | 1h-indazole-3-acetic acids as aldose reductase inhibitors |
| US4954629A (en) | 1989-05-11 | 1990-09-04 | Pfizer Inc. | Process and intermediates for the preparation of oxophthalazinyl acetic acids and analogs thereof |
| US4996204A (en) | 1989-05-11 | 1991-02-26 | Pfizer Inc. | Pyrido[2,3-d]pyridazinones as aldose reductase inhibitors |
| FR2647676A1 (fr) | 1989-06-05 | 1990-12-07 | Union Pharma Scient Appl | Nouveaux derives de pyridazinone, leurs procedes de preparation, medicaments les contenant, utiles notamment comme inhibiteurs de l'aldose reductase |
| US5304557A (en) | 1989-12-15 | 1994-04-19 | Pfizer Inc. | Substituted oxoophthalazinyl acetic acids and analogs thereof |
| JPH0495025A (ja) | 1990-08-08 | 1992-03-27 | Asahi Chem Ind Co Ltd | アルドースリダクターゼ阻害剤 |
| NZ254550A (en) * | 1992-09-28 | 1997-08-22 | Pfizer | Use of nitrogen-substituted pyrimidines to prepare medicaments useful for treatment or prevention of diabetic complications |
| BR9610207A (pt) | 1995-08-28 | 1999-02-02 | American Home Prod | Acidos fenóxi acéticos como inibidores da aldose redutase e agentes anti-hiperglicêmicos |
| EP1017697A1 (en) * | 1997-09-23 | 2000-07-12 | Novo Nordisk A/S | MODULES OF PROTEIN TYROSINE PHOSPHATASES (PTPases) |
| SK7522001A3 (en) | 1998-03-31 | 2002-02-05 | Inst For Pharm Discovery Inc | Substituted indolealkanoic acids |
| EP0982306A3 (en) | 1998-08-21 | 2000-07-05 | Pfizer Products Inc. | Polymorph of zopolrestat monohydrate |
| US6570013B2 (en) | 2000-02-16 | 2003-05-27 | Pfizer Inc | Salts of zopolrestat |
| ATE348100T1 (de) | 2001-03-30 | 2007-01-15 | Pfizer Prod Inc | Zwischenprodukten für die herstellung von pyridazinon aldose reductase inhibitoren. |
| JP2005527492A (ja) | 2002-01-23 | 2005-09-15 | イーライ・リリー・アンド・カンパニー | メラノコルチン受容体アゴニスト |
| US20040047919A1 (en) | 2002-06-13 | 2004-03-11 | Board Of Regents, The University Of Texas System | Methods and compositions involving aldose reductase inhibitors |
| AU2003242388A1 (en) * | 2002-06-14 | 2003-12-31 | Takeda Pharmaceutical Company Limited | Prodrug and process for producing the same |
| US7572910B2 (en) | 2003-02-20 | 2009-08-11 | Pfizer, Inc. | Pyridazinone aldose reductase inhibitors |
| US20070021366A1 (en) | 2004-11-19 | 2007-01-25 | Srivastava Satish K | Structural-based inhibitors of the glutathione binding site in aldose reductase, methods of screening therefor and methods of use |
| WO2006078717A2 (en) | 2005-01-19 | 2006-07-27 | Beth Israel Deaconess Medical Center | Lipocalin 2 for the treatment, prevention, and management of cancer metastasis, angiogenesis, and fibrosis |
| CN101143868A (zh) | 2007-09-04 | 2008-03-19 | 北京理工大学 | 醛糖还原酶抑制剂结构及用途 |
| PL2593456T3 (pl) | 2010-07-16 | 2017-06-30 | The Trustees Of Columbia University In The City Of New York | Inhibitory reduktazy aldozowej i ich zastosowania |
| US8916563B2 (en) | 2010-07-16 | 2014-12-23 | The Trustees Of Columbia University In The City Of New York | Aldose reductase inhibitors and uses thereof |
| CN102512407B (zh) | 2011-11-23 | 2014-05-21 | 中山大学 | 一种β-苯丙氨酸类化合物作为醛糖还原酶抑制剂的应用 |
| IL283809B2 (en) | 2016-06-21 | 2024-01-01 | Univ Columbia | Compounds for use in a method of treating neuropathy, retinopathy, nephropathy, or cardiomyopathy |
| US11329472B2 (en) | 2018-07-20 | 2022-05-10 | Texas Instruments Incorporated | Methods and apparatus to prevent undesired triggering of short circuit or over current protection |
-
2017
- 2017-06-21 IL IL283809A patent/IL283809B2/en unknown
- 2017-06-21 IL IL304979A patent/IL304979A/en unknown
- 2017-06-21 EP EP23201547.9A patent/EP4316603A3/en active Pending
- 2017-06-21 EP EP20188323.8A patent/EP3757107B1/en active Active
- 2017-06-21 EP EP17816127.9A patent/EP3352754B1/en active Active
- 2017-06-21 CN CN201780038647.5A patent/CN109310674B/zh active Active
- 2017-06-21 ES ES20188323T patent/ES2966094T3/es active Active
- 2017-06-21 HU HUE20188323A patent/HUE064911T2/hu unknown
- 2017-06-21 LT LTEP20188323.8T patent/LT3757107T/lt unknown
- 2017-06-21 HR HRP20231563TT patent/HRP20231563T1/hr unknown
- 2017-06-21 SI SI201730529T patent/SI3352754T1/sl unknown
- 2017-06-21 ES ES17816127T patent/ES2836500T3/es active Active
- 2017-06-21 DK DK20188323.8T patent/DK3757107T3/da active
- 2017-06-21 SG SG11201810642XA patent/SG11201810642XA/en unknown
- 2017-06-21 RS RS20201463A patent/RS61239B1/sr unknown
- 2017-06-21 JP JP2018567299A patent/JP6895464B2/ja active Active
- 2017-06-21 HR HRP20201905TT patent/HRP20201905T1/hr unknown
- 2017-06-21 SI SI201731462T patent/SI3757107T1/sl unknown
- 2017-06-21 PT PT201883238T patent/PT3757107T/pt unknown
- 2017-06-21 CN CN202210711329.3A patent/CN115160339B/zh active Active
- 2017-06-21 HU HUE17816127A patent/HUE052101T2/hu unknown
- 2017-06-21 FI FIEP20188323.8T patent/FI3757107T3/fi active
- 2017-06-21 AU AU2017281082A patent/AU2017281082B2/en active Active
- 2017-06-21 WO PCT/US2017/038505 patent/WO2017223179A1/en not_active Ceased
- 2017-06-21 MX MX2018016122A patent/MX391561B/es unknown
- 2017-06-21 PL PL20188323.8T patent/PL3757107T3/pl unknown
- 2017-06-21 DK DK17816127.9T patent/DK3352754T3/da active
- 2017-06-21 SG SG10202012188VA patent/SG10202012188VA/en unknown
- 2017-06-21 PT PT178161279T patent/PT3352754T/pt unknown
- 2017-06-21 LT LTEP17816127.9T patent/LT3352754T/lt unknown
- 2017-06-21 CA CA3025081A patent/CA3025081A1/en active Pending
-
2018
- 2018-04-24 US US15/961,288 patent/US10150779B2/en active Active
- 2018-11-06 US US16/182,169 patent/US10647726B2/en active Active
- 2018-12-10 IL IL263631A patent/IL263631B/en unknown
- 2018-12-18 ZA ZA2018/08506A patent/ZA201808506B/en unknown
- 2018-12-18 MX MX2021014938A patent/MX2021014938A/es unknown
-
2020
- 2020-03-31 US US16/835,876 patent/US10870658B2/en active Active
- 2020-11-02 US US17/086,699 patent/US11498925B2/en active Active
-
2021
- 2021-06-07 JP JP2021094883A patent/JP7368419B2/ja active Active
- 2021-06-09 AU AU2021203801A patent/AU2021203801B2/en active Active
-
2022
- 2022-10-13 US US18/046,205 patent/US12077547B2/en active Active
-
2023
- 2023-06-30 AU AU2023204218A patent/AU2023204218B2/en active Active
- 2023-10-12 JP JP2023176883A patent/JP7688681B2/ja active Active
-
2024
- 2024-07-23 US US18/781,034 patent/US20250163073A1/en active Pending
-
2025
- 2025-05-23 JP JP2025086125A patent/JP2025124733A/ja active Pending
- 2025-12-08 AU AU2025275331A patent/AU2025275331A1/en active Pending
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